Abstract: The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

Abstract: Disclosed are prodrugs of CGRP antagonists, methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof the prodrugs, pharmaceutical compositions comprising prodrugs and kits including the pharmaceutical compositions and instructions for use.

Abstract: The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I): or pharmaceutically acceptable salts thereof wherein R, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein. The disclosure also relates to methods of making and using compounds of Formula (I) or pharmaceutically acceptable salts thereof.

Abstract: A compound of the general formula (I), and the pharmaceutical composition including a compound of formula (I) and optionally a pharmaceutically acceptable additive. Also, the treatment of a cardiac disease, disorder or condition in a mammal, which includes the administration to the mammal a therapeutically effective amount of at least one compound of formula (I), or the pharmaceutically acceptable salt thereof.

Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Abstract: The present invention relates to compounds of Formula I as defined herein, and salts and solvates thereof. (I) The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to compounds of Formula (I) for use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which inhibition of a RAS-effector protein-protein interaction is implicated.

Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO2— or —SO2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R1

Abstract: Described herein are compounds, pharmaceutical compositions and methods of using these compounds and pharmaceutical compositions for treating and/or preventing conditions such as amyotrophic lateral sclerosis. These compounds and pharmaceutical compositions are also useful as antivirals and antimicrobial agents.

Abstract: The present invention relates to a novel method for preparing efinaconazole using an ionic liquid as a medium. The method includes subjecting 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole to a coupling reaction with 4-methylenepiperidine or an organic chemically acceptable salt thereof in the presence of a base and an ionic liquid compound. The base makes the 4-methylenepiperidine or organic chemically acceptable salt thereof anionic. The use of the ionic liquid in the method of the present invention prevents the formation of related substances, shortens the reaction time, and enables easy preparation of the final compound efinaconazole in high purity and yield on a large scale, compared to the use of organic solvents in conventional methods.

Abstract: Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

Abstract: Compounds of formula (I) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:

Abstract: A class of pyrimidoheterocyclic compounds, and specifically disclosed is a compound represented by formula (III) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: A reactive dye of formula wherein M is hydrogen, an alkali metal or one equivalent of an alkaline earth metal, Z1 is vinyl, ?-sulfatoethyl or the radical —NHCO—(CH2)3—SO2—CH2CH2Cl; R1 denotes H or sulfo; and R2 is H, methyl, methoxy or sulfo, n is the number 3; Y is vinyl or a radical —CH2—CH2-U and U is —Cl or —OSO3H, is suitable for dyeing and printing cellulosic or amide-group-containing fibre materials.

Abstract: Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

Abstract: The present invention relates to compounds according to general formula (I) which act as inhibitors of NaV1.8 and can be used in the treatment of pain.

Abstract: The present disclosure relates to the biopharmaceutical field, in particular, Exatecan derivatives, linker-payloads, and conjugates and thereof antibody-drug conjugates, and the corresponding preparing process and use thereof.

Abstract: Compositions and methods for co-administering curcumin and eucalyptol to a subject. Through the combined administration with eucalyptol, the plasma levels of curcumin will increase over the current baseline, thereby increasing the medicinal activity of the polyphenol and contributing to the reduction of an effective dose thereof, thereby also decreasing the incidence of side effects.

Abstract: The present invention relates to a pharmaceutical combination, comprising a glucokinase activator or a pharmaceutically acceptable salt, isotopic label, crystal form, hydrate, solvate, diastereomer, or enantiomer thereof and an SGLT-2 inhibitor. The present invention further relates to a pharmaceutical composition, a fixed-dose combination preparation, and preparation methods and uses thereof.

Abstract: The present invention is directed to compounds of formula I The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Parkinson's disease.